5378-94-9Relevant articles and documents
A novel class of ethacrynic acid derivatives as promising drug-like potent generation of anticancer agents with established mechanism of action
Mignani, Serge,El Brahmi, Nabil,El Kazzouli, Sa?d,Eloy, Laure,Courilleau, Delphine,Caron, Joachim,Bousmina, Mosto M.,Caminade, Anne-Marie,Cresteil, Thierry,Majoral, Jean-Pierre
, p. 656 - 673 (2016)
The well-known diuretic Ethacrynic acid (EA, Edecrin), showing low anti-proliferative activities, was chemically modified at different positions. The new EA derivatives have been tested in?vitro in anti-proliferative assays on both tumor KB (epidermal carcinoma) and leukemia HL60 (promyelocytic) cells suitable targets for anticancer activity. Reduction of the α-β double bond of EA completely abolished anti-cancer activities, whereas introduction of either 2-(4-substituted phenyl)ethanamine (series A) or 4-(4-substituted phenyl)piperazine (series B) moieties generated compounds showing moderate to strong anti-proliferative activities against human cancer cell lines. Several substitutions on the phenyl of these two moieties are tolerated. The mechanism of action of the EA derivatives prepared in this study is more complex than the inhibition of glutathione S-transferase π ascribed as unique effect to EA and might help to overcome tumor resistances.
Amide derivatives of ethacrynic acid: Synthesis and evaluation as antagonists of Wnt/β-catenin signaling and CLL cell survival
Jin, Guangyi,Lu, Desheng,Yao, Shiyin,Wu, Christina C.N.,Liu, Jerry X.,Carson, Dennis A.,Cottam, Howard B.
body text, p. 606 - 609 (2009/09/06)
A series of amides of ethacrynic acid was prepared and evaluated for their ability to inhibit Wnt signaling and decrease the survival of CLL cells. Several of the most potent derivatives were active in the low micromolar range. Reduction of the α,β-unsatu
